GSK1016790A
GSK1016790A, also known as GSK101, is a TRPV4 agonist that elicits calcium influx in HEK cells expressing mouse or human TRPV4 (EC50s = 18 and 2.1 nM, respectively).
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Chemical Information
| Name | GSK1016790A |
|---|---|
| Iupac Chemical Name | N-[(2S)-1-[4-[(2S)-2-[(2,4-dichlorophenyl)sulfonylamino]-3-hydroxypropanoyl]piperazin-1-yl]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamide |
| Synonyms | GSK1016790A; GSK-1016790A; GSK 1016790A; GSK101; GSK-101; GSK 101; |
| Molecular Formula | C28H32Cl2N4O6S2 |
| Molecular Weight | 655.61 |
| Smile | O=C(C1=CC2=CC=CC=C2S1)N[C@@H](CC(C)C)C(N3CCN(C([C@@H](NS(=O)(C4=CC=C(Cl)C=C4Cl)=O)CO)=O)CC3)=O |
| InChiKey | IVYQPSHHYIAUFO-VXKWHMMOSA-N |
| InChi | InChI=1S/C28H32Cl2N4O6S2/c1-17(2)13-21(31-26(36)24-14-18-5-3-4-6-23(18)41-24)27(37)33-9-11-34(12-10-33)28(38)22(16-35)32-42(39,40)25-8-7-19(29)15-20(25)30/h3-8,14-15,17,21-22,32,35H,9-13,16H2,1-2H3,(H,31,36)/t21-,22-/m0/s1 |
| CAS Number | 942206-85-1 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Addison MP, Singh TU, Parida S, Choudhury S, Kasa JK, Sukumaran SV, Darzi SA, Kandasamy K, Singh V, Kumar D, Mishra SK. NO synthase inhibition attenuates EDHF-mediated relaxation induced by TRPV4 channel agonist GSK1016790A in the rat pulmonary artery: Role of TxA2. Pharmacol Rep. 2016 Jun;68(3):620-6. doi: 10.1016/j.pharep.2016.01.003. PubMed PMID: 26991376.
2: Pankey EA, Zsombok A, Lasker GF, Kadowitz PJ. Analysis of responses to the TRPV4 agonist GSK1016790A in the pulmonary vascular bed of the intact-chest rat. Am J Physiol Heart Circ Physiol. 2014 Jan 1;306(1):H33-40. doi: 10.1152/ajpheart.00303.2013. PubMed PMID: 24186096; PubMed Central PMCID: PMC3920159.
3: Sullivan MN, Francis M, Pitts NL, Taylor MS, Earley S. Optical recording reveals novel properties of GSK1016790A-induced vanilloid transient receptor potential channel TRPV4 activity in primary human endothelial cells. Mol Pharmacol. 2012 Sep;82(3):464-72. doi: 10.1124/mol.112.078584. PubMed PMID: 22689561; PubMed Central PMCID: PMC3422704.
4: Jin M, Wu Z, Chen L, Jaimes J, Collins D, Walters ET, O'Neil RG. Determinants of TRPV4 activity following selective activation by small molecule agonist GSK1016790A. PLoS One. 2011 Feb 14;6(2):e16713. doi: 10.1371/journal.pone.0016713. PubMed PMID: 21339821; PubMed Central PMCID: PMC3038856.
5: Thorneloe KS, Sulpizio AC, Lin Z, Figueroa DJ, Clouse AK, McCafferty GP, Chendrimada TP, Lashinger ES, Gordon E, Evans L, Misajet BA, Demarini DJ, Nation JH, Casillas LN, Marquis RW, Votta BJ, Sheardown SA, Xu X, Brooks DP, Laping NJ, Westfall TD. N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1 -piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42. doi: 10.1124/jpet.108.139295. Erratum in: J Pharmacol Exp Ther. 2011 Jul;338(1):410. PubMed PMID: 18499743.
Chemical Structure
